EA201690935A1 - (AZA) PYRIDOPYRAZOLOPIRIMIDINONES AND INDAZOLOPIRIMIDINONES AS FIBRINOLYSIS INHIBITORS - Google Patents
(AZA) PYRIDOPYRAZOLOPIRIMIDINONES AND INDAZOLOPIRIMIDINONES AS FIBRINOLYSIS INHIBITORSInfo
- Publication number
- EA201690935A1 EA201690935A1 EA201690935A EA201690935A EA201690935A1 EA 201690935 A1 EA201690935 A1 EA 201690935A1 EA 201690935 A EA201690935 A EA 201690935A EA 201690935 A EA201690935 A EA 201690935A EA 201690935 A1 EA201690935 A1 EA 201690935A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- aza
- bleeding
- treating
- pyridopyrazolopirimidinones
- indazolopirimidinones
- Prior art date
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Настоящее изобретение относится к новым замещенным (аза)пиридопиразолопиримидинонам и индазолопиримидинонам, к способам их получения, к соединениям для применения по отдельности или в комбинации в способе лечения и/или профилактики заболеваний, в частности в способе лечения и/или профилактики острых и рецидивных кровотечений у пациентов с и без наследственных или приобретенных исходных нарушений свертываемости крови, когда указанное кровотечение связано с заболеванием или медицинским вмешательством, выбранным из группы, состоящей из меноррагии, послеродового кровотечения, геморрагического шока, травм, хирургического вмешательства, трансплантации, апоплексии, заболеваний печени, наследственного ангионевротического отека, носового кровотечения и синовита, а также повреждения хрящей вследствие гемартроза.The present invention relates to new substituted (aza) pyridopyrazolopyrimidinones and indazolopyrimidinones, to methods for their preparation, to compounds for use individually or in combination in a method of treating and / or preventing diseases, in particular in a method of treating and / or preventing acute and recurrent bleeding in patients with and without hereditary or acquired baseline bleeding disorders, when the indicated bleeding is associated with a disease or medical intervention selected from the group consisting of and menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, apoplexy, liver disease, hereditary angioedema, epistaxis and synovitis, as well as damage to cartilage due to hemarthrosis.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13191642 | 2013-11-05 | ||
| PCT/EP2014/073529 WO2015067549A1 (en) | 2013-11-05 | 2014-11-03 | (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones as inhibitors of fibrinolysis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201690935A1 true EA201690935A1 (en) | 2016-10-31 |
| EA029373B1 EA029373B1 (en) | 2018-03-30 |
Family
ID=49517406
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201690935A EA029373B1 (en) | 2013-11-05 | 2014-11-03 | (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones as inhibitors of fibrinolysis |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US9598417B2 (en) |
| EP (1) | EP3066100B1 (en) |
| JP (1) | JP6431061B2 (en) |
| KR (1) | KR102312780B1 (en) |
| CN (1) | CN105683194B (en) |
| AP (1) | AP2016009175A0 (en) |
| AR (1) | AR098292A1 (en) |
| AU (1) | AU2014345771B2 (en) |
| CA (1) | CA2929378C (en) |
| CL (1) | CL2016001076A1 (en) |
| CR (1) | CR20160332A (en) |
| CU (1) | CU24361B1 (en) |
| DO (1) | DOP2016000102A (en) |
| EA (1) | EA029373B1 (en) |
| ES (1) | ES2732305T3 (en) |
| GT (1) | GT201600084A (en) |
| HK (1) | HK1223940A1 (en) |
| IL (1) | IL244645B (en) |
| MA (1) | MA39018A1 (en) |
| MX (1) | MX370419B (en) |
| PE (1) | PE20160934A1 (en) |
| PH (1) | PH12016500828A1 (en) |
| SG (1) | SG11201602133RA (en) |
| TN (1) | TN2016000161A1 (en) |
| TW (1) | TWI657089B (en) |
| UA (1) | UA117504C2 (en) |
| UY (1) | UY35809A (en) |
| WO (1) | WO2015067549A1 (en) |
| ZA (1) | ZA201602311B (en) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY35809A (en) | 2013-11-05 | 2015-05-29 | Bayer Pharma AG | (AZA) PIRIDOPIRAZOLOPIRIMIDINONAS AND INDAZOLOPIRIMIDINONAS AND ITS USES |
| RU2713937C2 (en) * | 2014-11-03 | 2020-02-11 | Байер Фарма Акциенгезельшафт | Piperidinylpyrazolopyrimidinones and use thereof |
| WO2016173948A1 (en) * | 2015-04-30 | 2016-11-03 | Bayer Pharma Aktiengesellschaft | Indazolopyrimidinones as fibrinolysis inhibitors |
| WO2017007917A1 (en) * | 2015-07-07 | 2017-01-12 | Mast Therapeutics, Inc. | Polyoxyethylene/polyoxypropylene copolymers and fibrinolytic inhibitors, uses thereof and compositions |
| EP3318563A1 (en) | 2016-11-07 | 2018-05-09 | Sanofi | Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders |
| CN110590673A (en) * | 2019-09-02 | 2019-12-20 | 南通大学 | 4-chloro-7-methyl-1H-indazole and chemical synthesis method thereof |
| US11618751B1 (en) | 2022-03-25 | 2023-04-04 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives |
| US11654057B2 (en) | 2020-04-09 | 2023-05-23 | Bio 54, Llc | Devices for bleeding reduction and methods of making and using the same |
| EP4289850A1 (en) * | 2021-02-05 | 2023-12-13 | Scinnohub Pharmaceutical Co., Ltd | Plasmin inhibitor, preparation method therefor, and application thereof |
| CA3221317A1 (en) | 2021-06-09 | 2022-12-15 | David Anthony Barda | Substituted fused azines as kras g12d inhibitors |
| US11642324B1 (en) | 2022-03-01 | 2023-05-09 | Bio 54, Llc | Topical tranexamic acid compositions and methods of use thereof |
| AU2023251136A1 (en) | 2022-04-05 | 2024-10-17 | Bayer Aktiengesellschaft | Inhibitors of chymase for use in the selective resolution of thrombi in thrombotic or thromboembolic disorders |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2192559A5 (en) * | 1972-07-17 | 1974-02-08 | Ugine Kuhlmann | Pyrimidino (1,2-b) indazole derivs - inters for dyes and pharmaceuticals, from 3-aminoindazoles and beta-ketone derivs |
| JP5000504B2 (en) | 2004-07-30 | 2012-08-15 | フェリング ビー．ブイ． | Tranexamic acid preparation |
| AR059224A1 (en) * | 2006-01-31 | 2008-03-19 | Jerini Ag | COMPOUNDS FOR THE INHIBITION OF INTEGRINS AND USE OF THESE |
| CA2726554C (en) * | 2008-06-06 | 2015-02-24 | Sanofi-Aventis | Macrocyclic urea and sulfamide derivatives as inhibitors of tafia |
| US8691825B2 (en) | 2009-04-01 | 2014-04-08 | Merck Sharp & Dohme Corp. | Inhibitors of AKT activity |
| MX2011010647A (en) | 2009-04-07 | 2012-02-21 | Astrazeneca Ab | Isoxazol-3(2h)-one analogs as therapeutic agents. |
| WO2012047156A1 (en) * | 2010-10-04 | 2012-04-12 | Astrazeneca Ab | Isoxazol-3(2h)-one analogs as plasminogen inhibitors and their use in the treatment of fibrinolysis related diseases |
| US9132129B2 (en) * | 2010-11-15 | 2015-09-15 | Katholieke Universiteit Leuven | Antiviral compounds |
| WO2012082947A1 (en) * | 2010-12-16 | 2012-06-21 | Irm Llc | Compounds and compositions as tgr5 agonists |
| EP2651949B1 (en) * | 2010-12-16 | 2015-07-15 | Bayer Intellectual Property GmbH | Substituted pyrimido[1,2-b]indazoles and their use as modulators of the pi3k/akt pathway |
| UY35809A (en) | 2013-11-05 | 2015-05-29 | Bayer Pharma AG | (AZA) PIRIDOPIRAZOLOPIRIMIDINONAS AND INDAZOLOPIRIMIDINONAS AND ITS USES |
| WO2016173948A1 (en) * | 2015-04-30 | 2016-11-03 | Bayer Pharma Aktiengesellschaft | Indazolopyrimidinones as fibrinolysis inhibitors |
-
2014
- 2014-10-31 UY UY0001035809A patent/UY35809A/en not_active Application Discontinuation
- 2014-11-03 TN TN2016000161A patent/TN2016000161A1/en unknown
- 2014-11-03 EP EP14793523.3A patent/EP3066100B1/en active Active
- 2014-11-03 AU AU2014345771A patent/AU2014345771B2/en not_active Ceased
- 2014-11-03 UA UAA201605980A patent/UA117504C2/en unknown
- 2014-11-03 TW TW103137976A patent/TWI657089B/en not_active IP Right Cessation
- 2014-11-03 MX MX2016005969A patent/MX370419B/en active IP Right Grant
- 2014-11-03 WO PCT/EP2014/073529 patent/WO2015067549A1/en active Application Filing
- 2014-11-03 JP JP2016527398A patent/JP6431061B2/en not_active Expired - Fee Related
- 2014-11-03 ES ES14793523T patent/ES2732305T3/en active Active
- 2014-11-03 AP AP2016009175A patent/AP2016009175A0/en unknown
- 2014-11-03 PE PE2016000586A patent/PE20160934A1/en unknown
- 2014-11-03 EA EA201690935A patent/EA029373B1/en not_active IP Right Cessation
- 2014-11-03 CU CU2016000062A patent/CU24361B1/en unknown
- 2014-11-03 CN CN201480060660.7A patent/CN105683194B/en not_active Expired - Fee Related
- 2014-11-03 CR CR20160332A patent/CR20160332A/en unknown
- 2014-11-03 SG SG11201602133RA patent/SG11201602133RA/en unknown
- 2014-11-03 KR KR1020167014622A patent/KR102312780B1/en active IP Right Grant
- 2014-11-03 CA CA2929378A patent/CA2929378C/en not_active Expired - Fee Related
- 2014-11-03 MA MA39018A patent/MA39018A1/en unknown
- 2014-11-04 AR ARP140104130A patent/AR098292A1/en not_active Application Discontinuation
- 2014-11-05 US US14/533,915 patent/US9598417B2/en active Active
-
2016
- 2016-03-17 IL IL244645A patent/IL244645B/en active IP Right Grant
- 2016-04-06 ZA ZA2016/02311A patent/ZA201602311B/en unknown
- 2016-05-04 PH PH12016500828A patent/PH12016500828A1/en unknown
- 2016-05-05 CL CL2016001076A patent/CL2016001076A1/en unknown
- 2016-05-05 DO DO2016000102A patent/DOP2016000102A/en unknown
- 2016-05-05 GT GT201600084A patent/GT201600084A/en unknown
- 2016-10-27 HK HK16112345.9A patent/HK1223940A1/en not_active IP Right Cessation
-
2017
- 2017-01-26 US US15/416,651 patent/US10098883B2/en active Active
-
2018
- 2018-08-10 US US16/101,250 patent/US10668071B2/en not_active Expired - Fee Related
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AZ KG TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM BY KZ |